| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Ibt-DOX (25-50 nM; 1 hour) specifically releases free DOX in BTK-expressing OCI-LY10 cells, but has no effect in BTK-negative Jurkat cells [1]. Ibt-DOX (0-1000 nM; 1 hour) effectively inhibits the BTK-mediated BCR signaling pathway in OCI-LY10 cells, and completely blocks the phosphorylation of BTK and its downstream effector molecules at a concentration of 75 nM [1]. Ibt-DOX (0-400 nM; 20 hours) significantly induces the release of extracellular ATP and HMGB1 in BTK-expressing OCI-LY10 cells, but has no effect in BTK-negative Jurkat cells [1]. Ibt-DOX (0-100 μM; 72 hours) showed strong antiproliferative activity against OCI-LY10 and Ramos cells expressing BTK, while its activity was significantly reduced in BTK-negative cells, indicating that it has selective cytotoxicity against B-cell lymphoma cells expressing BTK[1].
|
|---|---|
| ln Vivo |
Ibt-DOX (2.5 mg/kg; intravenous injection; every 2 days; 14 days) reduced the volume of OCI-LY10 xenograft tumors in SCID mice by 54% and was well tolerated [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: OCI-LY10 Tested Concentrations: 75 nM Incubation Duration: 1 hour Experimental Results: Completely inhibited phosphorylation of BTK, PLCγ2, and Erk1/2. Phosphorylation of the upstream kinase Syk was unaffected. |
| Animal Protocol |
Animal/Disease Models:Female SCID mice were treated with OCI-LY10 cells [1].
Doses: 2.5 mg/kg Route of Administration: Intravenous injection; once every 2 days; for 14 days Experimental Results: The mean tumor volume was reduced by 54% compared with the control group. No significant changes in body weight or symptoms of toxicity were observed. |
| References |
| Molecular Formula |
C61H59N7O16
|
|---|---|
| Molecular Weight |
1146.16
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
NC1=C(C(C2=CC=C(C=C2)OC3=CC=CC=C3)=NN4[C@@H]5CCCN(C5)C(C(COC6=CC=C(C=C6)COC(N[C@H]7C[C@@H](O[C@@H](C)[C@H]7O)O[C@H]8C[C@@](O)(CC9=C8C(O)=C%10C(C(C%11=C(C%10=O)C(OC)=CC=C%11)=O)=C9O)C(CO)=O)=O)=C)=O)C4=NC=N1
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8725 mL | 4.3624 mL | 8.7248 mL | |
| 5 mM | 0.1745 mL | 0.8725 mL | 1.7450 mL | |
| 10 mM | 0.0872 mL | 0.4362 mL | 0.8725 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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